Solid phase synthesis of 1,4-benzothiazepin-5-one derivatives

Adel Nefzi, Nhi A. Ong, Marc A. Giulianotti, John M. Ostresh, Richard A. Houghten

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The solid phase synthesis of 1,4-benzothiazepin-5-one derivatives, resulting from the reaction of resin-bound protected cysteine with 2-fluoro- 5-nitro-benzoic acid followed by a reductive alkylation and an intra molecular cyclization, is described.

Original languageEnglish (US)
Pages (from-to)4939-4942
Number of pages4
JournalTetrahedron Letters
Issue number27
StatePublished - Jul 2 1999
Externally publishedYes

Bibliographical note

Funding Information:
ACKNOWLEDGEMENTS We thank Eileen Weiler for editorial assistance. This work was funded in part by National Science Foundation Grant No. CHE-9520142 (I-Ioughten) and National Cancer Institute Grant No. 1P01CA78040 (Houghten). REFERENCES AND NOTES 1. For reviews on solid phase organic synthesis, see: (a) Gallop, M. A.; Barret, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. Jr. Med, Chem.1 994, 37, 1233. (b) Gordon, E. M.; Barter, g. W.; Dower, W. J.;


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